Ravidasvir (RDV, ASC16) is a second‐generation, pan‐genotypic non‐structural (NS) 5A inhibitor, which inhibits viral replication and assembly. Ravidasvir exhibits high antiviral potency with EC50 0.04–1.14 nM for HCV GT1–GT6. The pharmacokinetics results indicated that steady status achieved quickly after the first dose. Metabolism studies utilizing human clinical samples showed that Ravidasvir was very stable, with only modest (~2%) metabolite formation. Biliary excretion of Ravidasvir appears to be the primary route of elimination of the absorbed dose, while renal excretion of the intact drug appears to be negligible. In clinical trans twelve-week Ravidasvir and ritonavir-boosted Danoprevir in combination with ribavirinfor 12 weeks achieve the sustained virologic response rate of 100% in treatment-naïve non-cirrhotic Asian patients with HCV GT1 infection. Ravidasvir for treatment‐naïve, non‐cirrhotic HCV GT1 patients was safe and well tolerated. There was no death, treatment‐related serious adverse events, and discontinued cases due to adverse events.

XL-888 is a highly potent and orally bioavailable ATP-competitive inhibitor of HSP90, a molecular chaperone protein that regulates the activity and stability of a range of key regulatory proteins, including a number of kinases implicated in cancer cell growth and survival. In preclinical studies, XL-888 has been shown to inhibit the proliferation of a broad panel of human tumor cell lines, and to induce marked degradation of HSP90 client proteins, including BRAF, MET, and HER2. XL-888 was discovered by Exelixis and is wholly owned by the company. XL-888 is currently in Phase I clinical trials for the treatment of malignant melanoma.

Golvatinib is a highly potent, small-molecule, ATP-competitive inhibitor of c-Met and multiple members of the Eph receptor family plus c-Kit and Ron. Eisai was developing an oral formulation of golvatinib, which acts as both a c-Met inhibitor and a vascular endothelial growth factor receptor 2 antagonist with potential antineoplastic activity. Golvatinib binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis. Clinical trials involving several forms of cancer are currently underway.

Valopicitabine is a nucleoside analog and the orally bioavailable prodrug of NM107 that competitively inhibits HCV NS5B polymerase, causing chain termination. Valopicitabine had been in phase II clinical trial for once-daily oral treatment of Hepatitis C virus infection. However, because of the overall risk/benefit profile of subjects undergoing clinical trials, further development of the drug has been temporarily placed on hold by the Swiss drug major Novartis and USA-based Idenix Pharmaceuticals company and the FDA.

PF-02413873 is a selective nonsteroidal progesterone receptor (PR) antagonist. PF-02413873 is turned over by recombinant human P450s, with CYP3A4 displaying the highest turnover of those enzymes tested. PF-02413873 possessed low oral clearance in human with a pharmacokinetic profile consistent with a once-daily dosing schedule. The pharmacological mode of action of PF-02413873 seems to differ from the founding member of the class of steroidal PR antagonists RU-486. Exposure-effect data from studies in the cynomolgus macaque, however, demonstrated that PF-02413873 reduced endometrial functionalis thickness to a comparable degree to RU-486 and this effect was accompanied by a decrease in proliferation rate for both RU-486 and high-dose PF-02413873. PF-02413873blocked the follicular phase increase in endometrial thickness, the midcycle luteinizing hormone surge, and elevation in estradiol in a dose-dependent fashion compared with placebo. PF-02413873 had been in phase I clinical trial for the treatment of endometriosis. However, this development was discontinued.

PF-04217903 is a triazolopyrazine inhibitor of c-MET that displays anticancer chemotherapeutic and anti-metastatic activities. PF-04217903 inhibits cell proliferation, invasion, and migration as well as tumor growth in various cancer models. In animal models of pancreatic neuroendocrine tumors, this compound prevents lymph node metastasis. PF-04217903 had been in phase I clinical trials by Pfizer for the treatment of solid tumors. In 2011, the company discontinued the development of the compound.

Navarixin (SCH 527123) is an oral antagonist of CXC receptors 1 and 2. The drug is currently under Phase II trial for the treatment of psoriasis, COPD and asthma.